TWI472513B - A quinolyl-containing hydroxamic acid-based compound and a process for preparing the same, and a method for producing the same Pharmaceutical compositions and their use - Google Patents

A quinolyl-containing hydroxamic acid-based compound and a process for preparing the same, and a method for producing the same Pharmaceutical compositions and their use Download PDF

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Publication number
TWI472513B
TWI472513B TW101128702A TW101128702A TWI472513B TW I472513 B TWI472513 B TW I472513B TW 101128702 A TW101128702 A TW 101128702A TW 101128702 A TW101128702 A TW 101128702A TW I472513 B TWI472513 B TW I472513B
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Taiwan
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methoxy
oxy
phenyl
fluorophenyl
cyclopropane
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TW101128702A
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English (en)
Chinese (zh)
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TW201313683A (zh
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Konruns Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
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    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurosurgery (AREA)
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  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
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TW101128702A 2011-09-19 2012-08-09 A quinolyl-containing hydroxamic acid-based compound and a process for preparing the same, and a method for producing the same Pharmaceutical compositions and their use TWI472513B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201110278403.9A CN102408411B (zh) 2011-09-19 2011-09-19 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用

Publications (2)

Publication Number Publication Date
TW201313683A TW201313683A (zh) 2013-04-01
TWI472513B true TWI472513B (zh) 2015-02-11

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TW101128702A TWI472513B (zh) 2011-09-19 2012-08-09 A quinolyl-containing hydroxamic acid-based compound and a process for preparing the same, and a method for producing the same Pharmaceutical compositions and their use

Country Status (13)

Country Link
US (1) US9186318B2 (fr)
EP (1) EP2769976B8 (fr)
JP (1) JP5795826B2 (fr)
KR (1) KR101879908B1 (fr)
CN (1) CN102408411B (fr)
AU (1) AU2011377440B2 (fr)
CA (1) CA2858033C (fr)
HK (1) HK1171009A1 (fr)
NZ (1) NZ623923A (fr)
RU (1) RU2573633C2 (fr)
SG (1) SG11201400769PA (fr)
TW (1) TWI472513B (fr)
WO (1) WO2013040801A1 (fr)

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CN103748074B8 (zh) * 2011-06-17 2016-09-14 南昌弘益药业有限公司 芳氧基喹啉类衍生物及其治疗用途
CA2964106C (fr) 2012-04-23 2018-10-02 Nemaska Lithium Inc. Procedes de preparation d'hydroxyde de lithium
WO2013177367A2 (fr) 2012-05-23 2013-11-28 The Johns Hopkins University Composés et méthodes d'utilisation de ceux-ci pour traiter des troubles neurodégénératifs
CA2927020C (fr) 2012-05-30 2021-03-23 Nemaska Lithium Inc. Procedes de preparation de carbonate de lithium
WO2014138933A1 (fr) 2013-03-15 2014-09-18 Nemaska Lithium Inc. Procédés pour la préparation d'hydroxyde de lithium
SG10201804835VA (en) 2013-10-11 2018-07-30 Alios Biopharma Inc Substituted nucleosides, nucleotides and analogs thereof
KR102132463B1 (ko) 2013-10-23 2020-08-06 네마스카 리튬 인코포레이션 리튬 카보네이트의 제조방법
CA2938818C (fr) * 2014-02-04 2023-03-07 Astellas Pharma Inc. Composition pharmaceutique comprenant un compose carboxamide heterocyclique diamine en tant que principe actif
CA3005843C (fr) 2014-02-24 2019-08-13 Nemaska Lithium Inc. Procedes pour le traitement de materiaux contenant du lithium
WO2016183071A1 (fr) 2015-05-11 2016-11-17 Incyte Corporation Composés hétéro-tricycliques substitués et utilisation de ces composés pour le traitement du cancer
SI3322706T1 (sl) 2015-07-16 2021-04-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze
WO2017027717A1 (fr) 2015-08-12 2017-02-16 Incyte Corporation Composés de pyrimidine fusionnés bicycliques utilisés en tant qu'inhibiteurs de tam
WO2017035366A1 (fr) 2015-08-26 2017-03-02 Incyte Corporation Dérivés de type pyrrolo-pyrimidine utilisés comme inhibiteurs des tam
SG11201808582RA (en) 2016-03-28 2018-10-30 Incyte Corp Pyrrolotriazine compounds as tam inhibitors
CN107778285A (zh) * 2016-08-24 2018-03-09 南昌弘益药业有限公司 一类喹啉类新化合物
CA2940509A1 (fr) 2016-08-26 2018-02-26 Nemaska Lithium Inc. Procede de traitement de compositions aqueuses comprenant du sulfate de lithium et de l'acide sulfurique
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
AU2017346104B2 (en) * 2016-10-18 2020-06-11 Beijing Konruns Pharmaceutical Co., Ltd. Quinolinyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition thereof, and use thereof
CN108329298A (zh) * 2017-01-17 2018-07-27 南昌弘益药业有限公司 一类喹啉类新化合物制备方法
WO2018136663A1 (fr) 2017-01-18 2018-07-26 Array Biopharma, Inc. Inhibiteurs de ret
ES2948194T3 (es) 2017-01-18 2023-09-01 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN108623565A (zh) * 2017-03-23 2018-10-09 南昌弘益药业有限公司 一种化合物的制备方法
US11149021B2 (en) * 2017-05-24 2021-10-19 Abbisko Therapeutics Co., Ltd. N-(azaaryl)cyclolactam-1-carboxamide derivative, preparation method therefor, and use thereof
PT3687996T (pt) 2017-09-27 2022-01-21 Incyte Corp Sais de derivados de pirrolotriazina úteis como inibidores de tam
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
US11401260B2 (en) * 2017-10-20 2022-08-02 Kala Pharmaceuticals, Inc. Biochemical binding of RET9 and VEGFR2 inhibitors
CA3083136C (fr) 2017-11-22 2022-04-12 Nemaska Lithium Inc. Procedes de preparation d'hydroxydes et d'oxydes de divers metaux et leurs derives
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